Mafenide
(Synonyms: 磺胺米隆) 目录号 : GC36528
A sulfonamide antibiotic
Cas No.:138-39-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Mafenide is a sulfonamide antibiotic that inhibits growth of bacteria.1,2 It inhibits growth of clinical isolates of S. pyogenes, methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. aureus (MRSA), Enterococcus, Enterobacteriaceae, and Gram-negative bacilli from burn patients in an agar well diffusion assay (mean zone of inhibition = 24-37 mm) but not in a broth dilution assay with MIC values ranging from 250 to greater than 5,000 μg/ml.1 Mafenide also inhibits growth of clinical isolates of K. pneumoniae that produce extended spectrum β-lactamase (ESBL), P. aeruginosa, and A. baumannii-calcoaceticus from burn patients in an agar well diffusion assay (mean zones of inhibition = 23.5, 28.9, and 25.8 mm, respectively) but not in a broth dilution assay (mean MICs = 1,024 μg/ml, 1,024 μg/ml, and 1,024 μg/ml, respectively).2 It decreases mortality in a rat model of burn wounds seeded with rat virulent P. aeruginosa.3 Mafenide also inhibits human carbonic anhydrase (CA) I and II (Kis = 41.91 and 0.612 μM, respectively).4 Formulations containing mafenide have been used in the treatment of severe burns.
1.Rodgers, G.L., Mortensen, J.E., Fisher, M.C., et al.In vitro susceptibility testing of topical antimicrobial agents used in pediatric burn patients: Comparison of two methodsJ. Burn Care Rehabil.18(5)406-410(1997) 2.Glasser, J.S., Guymon, C.H., Mende, K., et al.Activity of topical antimicrobial agents against multidrug-resistant bacteria recovered from burn patientsBurns36(8)1172-1184(2010) 3.Fox, C.L., Jr., Sampath, A.C., and Stanford, J.W.Virulence of Pseudomonas infection in burned rats and mice. Comparative efficacy of silver sulfadiazine and mafenideArch. Surg.101(4)508-512(1970) 4.Fidan, ?., Salmas, R.E., Arslan, M., et al.Carbonic anhydrase inhibitors: Design, synthesis, kinetic, docking and molecular dynamics analysis of novel glycine and phenylalanine sulfonamide derivativesBioorg. Med. Chem.23(23)7353-7358(2015)
| Cas No. | 138-39-6 | SDF | |
| 别名 | 磺胺米隆 | ||
| Canonical SMILES | O=S(C1=CC=C(CN)C=C1)(N)=O | ||
| 分子式 | C7H10N2O2S | 分子量 | 186.23 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml,Ethanol: slightly soluble | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.3697 mL | 26.8485 mL | 53.697 mL |
| 5 mM | 1.0739 mL | 5.3697 mL | 10.7394 mL |
| 10 mM | 0.537 mL | 2.6849 mL | 5.3697 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Topical Mafenide hydrochloride aqueous spray in initial management of massive contaminated wounds with devitalized tissue
Prehosp Disaster Med 2001 Jul-Sep;16(3):172-4.PMID:11875802DOI:10.1017/s1049023x00025930.
Since at least WWII, some open, contaminated wounds involving massive soft tissue injury and vascular damage have resulted in "irreversible shock," despite prompt rescue, hemorrhage control, and blood and fluid replacement, without signs of clinical infection. In animal studies, survival time was related statistically to the dosage of Clostridium perfringens in multicontaminated explosive wounds. Survival time was lengthened by the application of some topical antibacterial agents, but actual recovery was achieved only with topical Mafenide hydrochloride solution aqueous spray, which resulted in negative clostridium. perfringens cultures. Although not related statistically to survival time, the Mafenide hydrochloride spray also controlled the Pseudomonas aeruginosa in these wounds. Mafenide hydrochloride had the American trade name of Sulfamylon from about 1942 until 1998, when another pharmaceutical company patented Sulfamylon as the trade name for Mafenide acetate, a weaker antibacterial agent. However, Mafenide hydrochloride still is available from chemical companies. Mafenide hydrochloride solution spray has been used successfully in treatment of patients with severe by contaminated wounds and deep burns, and its use in initial care should be revisited.
Allergic contact dermatitis to Mafenide acetate: a case series and review of the literature
J Drugs Dermatol 2007 Aug;6(8):825-8.PMID:17763614doi
Burn patients with extensive involvement of body surface area (BSA >30%) represent a challenge in wound treatment. Multiple topical agents may be used for cleansing, barrier protection, and antimicrobial control leading to complications of contact and/or irritant dermatitis, which may further complicate re-epithelization and eventual wound healing. We present 4 patients who sustained extensive burns during Operation Iraqi Freedom/Operation Enduring Freedom and later developed contact dermatitis to Mafenide acetate, a common topical antimicrobial used in burn care treatment, also known as Sulfamylon (alpha-amino-p-toluenesulfonamide monoacetate). All patients who were patch tested to Mafenide acetate 7% solution were positive. A rechallenge with Mafenide acetate resulted in recrudescence of the eruption in 2 out of the 4 patients. Though cutaneous reactions to Mafenide acetate were reported by Yaffe and Dressler in 1969, the most recent case reports are from 1995. This paper presents more recent examples of cutaneous reactions to Mafenide acetate, while also reviewing the literature.
Mafenide derivatives inhibit neuroinflammation in Alzheimer's disease by regulating pyroptosis
J Cell Mol Med 2021 Nov;25(22):10534-10542.PMID:34632701DOI:10.1111/jcmm.16984.
The main mechanism of pyroptosis is Caspase-1-mediated GSDMD cleavage, and GSDMD is also the executive protein of pyroptosis. Our previous study has shown that Mafenide can inhibit pyroptosis by inhibiting the GSDMD-Asp275 site to suppress cleavage. In this study, sulfonamide was used as the parent nucleus structure to synthesize sulfa-4 and sulfa-20. Screening of drug activity in the pyroptosis model of BV2 and iBMDM cell lines revealed the efficacy of five compounds were superior to Mafenide, which exerted a better inhibitory effect on the occurrence of pyroptosis. For in vivo assay, Sulfa-4 and Sulfa-22 were intervened in the neuroinflammation APP/PS1 mice. As a result, the administration of Sulfa-4 and Sulfa-22 could significantly inhibit the activation of microglia, decrease the expression of inflammatory factors in the central nervous system and simultaneously suppress the production of p30-GSDMD as well as the expression of upstream NLRP3 inflammasome and Caspase-1 protein. Immunoprecipitation and Biotin-labelled assay confirmed the targeted binding relationship of Sulfa-4 and Sulfa-22 with GSDMD protein in the iBMDM model in vitro. In this study, we investigated a new type inhibitor of GSDMD cleavage, which exerted a good inhibitory effect on pyroptosis and provided new references for the development of inflammatory drugs in the future.
The downside of antimicrobial agents for wound healing
Eur J Clin Microbiol Infect Dis 2019 Jan;38(1):39-54.PMID:30291466DOI:10.1007/s10096-018-3393-5.
The use of topical antimicrobials is beneficial for infection control in wound care because wound infection is the major cause of delayed healing. The advantages of topical over systemic antimicrobials include a higher concentration at the target site, fewer systemic adverse effects, and a lower incidence of antimicrobial resistance. Nowadays, topical antimicrobials are divided into three groups: disinfectants, antiseptics, and antibiotics. Only antiseptics and antibiotics can be applied to living skin; therefore, this review will focus only on these groups. The advantages of each topical antimicrobial are well established; however, their disadvantages remain prominent. It is widely known that antiseptics show higher cytotoxicity and a broader spectrum of activity than antibiotics, whereas antibiotics show a higher probability of bacterial resistance development. However, there are still many adverse effects, resulting from each topical antimicrobial. This review aims to summarize the possible adverse effects of commonly used antiseptics (biguanide, silver, iodine, chlorine compounds, and other antiseptics), antibiotics (bacitracin, Mafenide, mupirocin, neomycin, and silver sulfadiazine), and natural antimicrobials (curcumin and honey). Moreover, the antimicrobials that should be avoided in particular populations are also summarized in this review in order to increase awareness for antimicrobial selection in those populations.
Thermal stability of Mafenide and amphotericin B topical solution
Burns 2018 Mar;44(2):475-480.PMID:28935221DOI:10.1016/j.burns.2017.08.019.
Objective: Fungal infections remain a major cause of mortality in the burned population. Mafenide acetate/amphotericin B solution (SMAT) has been used topically for prophylaxis and treatment of these infections. Current manufacturer guidelines only guarantee the stability of Mafenide solution and amphotericin B at room temperature. Additionally, the recommended maximum storage time for Mafenide solution is 48h, leading to significant financial and material loss when unused solutions are discarded. The purpose of this study was to characterize the chemical stability, structure and bioactivity of SMAT stored at 2°C, 25°C, and 40°C for up to 90 days. Methods: Stability analyses of SMAT solutions containing 2.5% or 5% Mafenide plus 2μg/mL amphotericin B were performed using high performance liquid chromatography. Chemical structure was assessed using Fourier-transform infrared spectroscopy. Bioactivity against clinically relevant species was examined. Results: The chemical structure and stability of Mafenide did not change over 90days at all temperatures. Amphotericin B was undetectable in SMAT solutions after two days at high temperatures, which was slowed by refrigerated storage. Against Staphylococcus aureus, SMAT activity began to decrease generally between two and seven days. Against Pseudomonas aeruginosa, activity slowly tapered and was gone by day 90. SMAT retained high bioactivity against Candida albicans for over 40days and was not affected by temperature. Conclusions: The amphotericin B component of SMAT is degraded within 2days under warm storage. While Mafenide was stable over 90 days, the bioactivity of SMAT solution may be lost within 2days as well.